Asian Journal of Organic & Medicinal Chemistry最新文献_第10页

Synthesis, Characterization, Antimicrobial Screening of 5-Bromobenzofuranyl Aryl Ureas and Carbamates 5-溴苯并呋喃基脲基氨基甲酸酯的合成、表征及抗菌筛选

Asian Journal of Organic & Medicinal Chemistry Pub Date : 2019-01-01 DOI: 10.14233/ajomc.2019.ajomc-p215

H. M. N. Kumari, Manjunath Harihara Mathada, Mahesh Kumar, K. Suda, K. Basavaraja

引用次数: 0

Design, Optimization and Evaluation of Lurasidone Hydrochloride Nanocrystals as Fast Disintegrating Tablets 盐酸鲁拉西酮纳米晶快速崩解片的设计、优化及评价

Asian Journal of Organic & Medicinal Chemistry Pub Date : 2019-01-01 DOI: 10.14233/AJOMC.2019.AJOMC-P209

Satyanarayan Sahoo, C. B. Rao

{"title":"Design, Optimization and Evaluation of Lurasidone Hydrochloride Nanocrystals as Fast Disintegrating Tablets","authors":"Satyanarayan Sahoo, C. B. Rao","doi":"10.14233/AJOMC.2019.AJOMC-P209","DOIUrl":"https://doi.org/10.14233/AJOMC.2019.AJOMC-P209","url":null,"abstract":"Formulation of poorly water-soluble drugs for oral drug delivery has always been a difficult task for formulation scientists. Lurasidone hydrochloride is one such agent which is used to control bipolar depre-ssion. The objective of this study was to formulate and optimize lurasi-done nanosuspension, further formulating optimized nanosuspensions as fast disintegrating tablets for improved patient compliance. In the present study, lurasidone nanosuspension was prepared by nanomilling technique. Optimized nanosuspension has mean particle diameter of 248.9 nm, polydispersity index of 0.127 and zeta potential of 18.1 mV. The lyophilized optimized nanocrystals, optimize nanosuspension as granulating fluid and as top spraying dispersion for granulation in fluid bed granulator being used to formulate fast disintegrating tablets with suitable super disintegrant. Croscarmellose sodium was found to be best superdisintegrant compared to sodium starch glycolate and crospovidone, as its acts by both mechanism swelling and wicking. Its swells 4-8 folds in less than 10 s. Many folds increase in the rate of drug release observed compare to micronized lurasidone and marketed product. There was no change in crystalline nature after nanomilling as characterized by XRD and FTIR, and it was found to be chemically stable with high drug content. The developed fast disintegrating tablets would be an alternative better formulation than its conventional formulation to address its bioavailability issue and for improved patient compliance. However, this should be further confirmed by appropriate in vivo studies.","PeriodicalId":8846,"journal":{"name":"Asian Journal of Organic & Medicinal Chemistry","volume":"36 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"85052746","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

in silico Docking Analysis of Small Molecule Inhibitors fromNyctanthes arbor-tristis against Nipah Virus Infection 尼帕病毒小分子抑制剂的硅对接分析

Asian Journal of Organic & Medicinal Chemistry Pub Date : 2019-01-01 DOI: 10.14233/ajomc.2019.ajomc-p235

N. Mohan, V. Meera, J. Soja, M. Latha

{"title":"in silico Docking Analysis of Small Molecule Inhibitors from\u0000Nyctanthes arbor-tristis against Nipah Virus Infection","authors":"N. Mohan, V. Meera, J. Soja, M. Latha","doi":"10.14233/ajomc.2019.ajomc-p235","DOIUrl":"https://doi.org/10.14233/ajomc.2019.ajomc-p235","url":null,"abstract":"Nipah virus is a highly pathogenic paramyxovirus belonging to the genus Henipavirus, classified as Biosafety Level 4 (BSL4) agents. The virus causes severe illness characterized by encephalitis or respiratory disease in human. The case-lethality rate of Nipah was reported to be 70 % in India, since year 2001. Despite the high pathogenicity of virus, no therapeutics are currently approved for use in human. But, ribavirin, favipiravir and human mono clonal antibody was found to reduce the intensity in early stage. Medicinal plants serve as a rich source of therapeutically active compounds. Nyctanthus arbortristis Linn or pavizhamalli (Harsinger) is traditionally known to have activity against Nipha virus. In this study, therapeutic activity of phytochemicals arbortristoside A and arbortristoside C present in pavizhamalli plant against Nipha virus target was investigated by computational docking simulation. Computational docking analysis was performed using Schrodinger Suite. The phytochemicals arbortristoside A and arbortristoside C show promising binding affinity with the target Nipah virus than the reference drugs. Results of the study could be advantageous to develop a new lead molecule against Nipah virus infection.","PeriodicalId":8846,"journal":{"name":"Asian Journal of Organic & Medicinal Chemistry","volume":"80 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"82363466","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Synthesis and Antifungal Activity of New Dihydropyrazoles of Designed Curcumin Analogues 新型姜黄素类似物双氢吡唑的合成及抗真菌活性研究

Asian Journal of Organic & Medicinal Chemistry Pub Date : 2019-01-01 DOI: 10.14233/AJOMC.2019.AJOMC-P179

V. Tripathi, N. Saxena

引用次数: 1

Synthesis of Novel Substituted 1,5-Benzothiazepines Containing 1,4-Benzodioxane Sulfonyl Moiety 含1,4-苯二氧环磺酰基的新型取代1,5-苯并噻唑类化合物的合成

Asian Journal of Organic & Medicinal Chemistry Pub Date : 2019-01-01 DOI: 10.14233/AJOMC.2019.AJOMC-P159

Sandhya Chhakra, A. Mukherjee, Harlal Singh, S. Chauhan

{"title":"Synthesis of Novel Substituted 1,5-Benzothiazepines Containing 1,4-Benzodioxane Sulfonyl Moiety","authors":"Sandhya Chhakra, A. Mukherjee, Harlal Singh, S. Chauhan","doi":"10.14233/AJOMC.2019.AJOMC-P159","DOIUrl":"https://doi.org/10.14233/AJOMC.2019.AJOMC-P159","url":null,"abstract":"An efficient synthesis of novel 2,3,4-trisubstituted 1,5-benzothiazepines (4a-e) incorporating the sulfonyl group is described. Compound (4a-e) was synthesized by the reaction of 3-(1,4-dioxane-6-sulfonyl)-2,4-dimethyl/4-methyl-2-phenyl/2,4-diphenyl/2-ethoxy-4-methyl/2,4-diethoxy propane-1,3-dione (3ae) with 2-aminobenzenethiol with ZnOnanoparticles/pyridine. Formation of compound (3a-e) was achieved by the reaction of 1,4-dioxane-6-sulfonyl chloride (1) with 2,4-dimethyl/4-methyl-2-phenyl/2,4-diphenyl/2-ethoxy-4-methyl/2,4-diethoxy propane-1,3-dione (2a-e). The benzothiazepines (4a-e) obtained were purified by column chromatography (benzene: CHCl3, 40:60, 30:70, 20:80, 10:90) and crystallized from methanol. The purity of the compounds was checked by TLC using (CHCl3: CH3OH, 9:1) as the mobile phase. The structure of the compounds has been established by elemental, IR, 1H NMR, 13C NMR and Mass spectral analyses. Frontier molecular orbitals of the title compounds have been studied in the ground state speculatively. The reactivity of a molecule using diverse descriptors such as softness, electrophilicity, electronegativity, HOMO-LUMO energy gap is calculated additionally discussed.","PeriodicalId":8846,"journal":{"name":"Asian Journal of Organic & Medicinal Chemistry","volume":"33 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"87948380","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Synthesis and Antibacterial Study of Novel Piperazine Linked Methylene-bis-Coumarins 新型哌嗪类亚甲基双香豆素的合成及抗菌研究

Asian Journal of Organic & Medicinal Chemistry Pub Date : 2019-01-01 DOI: 10.14233/ajomc.2019.ajomc-p177

A. Nagaraj, S. Srinivas, P. R. Naik, R. Neelofer

引用次数: 0

Designing of Nitroimidazole Derivatives as a Promising Target for Treatment of Tuberculosis 硝基咪唑衍生物作为治疗结核病有前景的靶点的设计

Asian Journal of Organic & Medicinal Chemistry Pub Date : 2019-01-01 DOI: 10.14233/AJOMC.2019.AJOMC-P173

Monika Kakadiya, S. Ramiya, M. Noolvi, T. Pasha

{"title":"Designing of Nitroimidazole Derivatives as a Promising Target for Treatment of Tuberculosis","authors":"Monika Kakadiya, S. Ramiya, M. Noolvi, T. Pasha","doi":"10.14233/AJOMC.2019.AJOMC-P173","DOIUrl":"https://doi.org/10.14233/AJOMC.2019.AJOMC-P173","url":null,"abstract":"Tuberculosis is an infectious disease caused by Mycobacterium tuberculosis, with high level of mortality worldwide, currently with approximately 10 million cases of tuberculosis. These rate of incidence are due to several factors such as bacterial resistance, AIDS, latent tuberculosis that reoccur in patient. Deazaflavin dependent nitroreductase (Ddn) is an emerging target in the field of antitubercular agent. Ddn catalyses the reduction of nitroimidazoles resulting in intra-cellular release of lethal reactive nitrogen species. Nitroimidazole class drug- delamanid and pretonamid are used in the treatment of MDR-TB. In this present study, 26 new nitroimidazole derivatives were designed and docked into Ddn enzyme. In docking study, compounds 3, 5, 15, 16, 17, 18 and 21 showed similar interaction with amino acid residues such as Tyr 65, Ser 78, Tyr 136 as pretonamid reference drug and highest docking score and better ADMET compatibility. The ADMET prediction docking study of new designed compound revealed that the compounds 3, 16, 17 and 21 showed good binding with Ddn. In future it may be good and effective lead for development of antitubercular agent.","PeriodicalId":8846,"journal":{"name":"Asian Journal of Organic & Medicinal Chemistry","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"89510860","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Synthesis and Antimicrobial Activity of Azobenzene Based Titania Nanoparticles Coated Cotton Fibers 偶氮苯基纳米二氧化钛包覆棉纤维的合成及抗菌性能研究

Asian Journal of Organic & Medicinal Chemistry Pub Date : 2019-01-01 DOI: 10.14233/AJOMC.2019.AJOMC-P144

Mamta Sharma, S. Tomar

引用次数: 0

A Novel and Facile Synthesis of Thiopyrimidines and O-Glucosides 一种新型简便的硫代嘧啶和o -糖苷合成方法

Asian Journal of Organic & Medicinal Chemistry Pub Date : 2019-01-01 DOI: 10.14233/AJOMC.2019.AJOMC-P161

R. Wanare

引用次数: 1

Synthesis, Characterization, Crystal and Molecular Structure Analysis of1-(2-Chlorophenyl)-3-methyl-4-(p-tolylthio)-1H-pyrazol-5-ol 1-(2-氯苯基)-3-甲基-4-(对甲基硫)- 1h -吡唑-5-醇的合成、表征、晶体及分子结构分析

Asian Journal of Organic & Medicinal Chemistry Pub Date : 2019-01-01 DOI: 10.14233/ajomc.2019.ajomc-p189

R. Kamani, Rahul P. Thummar, Nirav H. Sapariya, Beena K. Vaghasiya, Jemin R. Avalani, Vishal B. Purohit, K. Patel, Dipak K. Raval

引用次数: 0